l General Information |
Product Name | PF-03549184 |
General description | PF-03549184 (PF-9184) is a potent inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1). |
Synonym | PF-9184; N-(3′,4′-dichloro[1,1′-biphenyl]-4-yl)-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide |
Purity | ≥98.0%(HPLC) | CAS Number | 1221971-47-6 |
Formula | C21H14Cl2N2O4S | Molecular Weight | 461.32 |
Suitability | BioReagent, suitable for cell culture, etc. |
l Physical and Chemical Information |
Appearance | White to beige Solid |
Solubility(25℃) | DMSO | ~5mg/mL(warmed) |
l Biological Information |
Biochem/Physiol Actions | PF-03549184 (PF-9184) is a potent inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1) with an IC50 value of 16.5 nM in recombinant human mPGES-1. mPEGS-1 is the terminal enzyme that synthesizes prostaglandin E2 (PGE2) from PGH2 to PGE2 downstream of cyclooxygenase-2 (COX-2). Its is induced in response to pro-inflammatory mediators, similar to COX-2. Unlike the effects of COX inhibition, PF-9184 does not inhibit the production of other PGH2-derived products such as 6-keto-PGFα or PGF2α. PF-9184 inhibits PGE2 production in cell based assays with IC50 ranges from 0.5 to 5 μM. IC50 concentrations for rhCOX1 and rHCOX2 are 118 μM and 236 μM, respectively. PGE2 is involved in inflammation and is one of the most abundant prostanoid. |
l Storage |
Storage temp. | -20℃ |
l Precautions and Disclaimer |
This product is for R&D use only, not for drug, household, or other uses. |
l References |
1. http://www.drugbank.ca 2. https://ncit.nci.nih.gov 3. https://www.ncbi.nlm.nih.gov |
